CN113563311A - 用作雄激素受体拮抗剂的二芳基硫代乙内酰脲化合物 - Google Patents

用作雄激素受体拮抗剂的二芳基硫代乙内酰脲化合物 Download PDF

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CN113563311A
CN113563311A CN202110901351.XA CN202110901351A CN113563311A CN 113563311 A CN113563311 A CN 113563311A CN 202110901351 A CN202110901351 A CN 202110901351A CN 113563311 A CN113563311 A CN 113563311A
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compound
alkyl
hydroxy
independently selected
synthesis
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沈春莉
吴成德
陈胜林
陈曙辉
张喜全
田心
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Chia Tai Tianqing Pharmaceutical Group Co Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41781,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
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    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN202110901351.XA 2017-08-07 2018-08-07 用作雄激素受体拮抗剂的二芳基硫代乙内酰脲化合物 Pending CN113563311A (zh)

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CN2017106678604 2017-08-07
CN201710667860 2017-08-07
CN201810333652 2018-04-13
CN2018103336525 2018-04-13
CN201880055633.9A CN111032644B (zh) 2017-08-07 2018-08-07 用作雄激素受体拮抗剂的二芳基硫代乙内酰脲化合物

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CN202110900404.6A Active CN113582977B (zh) 2017-08-07 2018-08-07 用作雄激素受体拮抗剂的二芳基硫代乙内酰脲化合物
CN201880055633.9A Active CN111032644B (zh) 2017-08-07 2018-08-07 用作雄激素受体拮抗剂的二芳基硫代乙内酰脲化合物

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CN201880055633.9A Active CN111032644B (zh) 2017-08-07 2018-08-07 用作雄激素受体拮抗剂的二芳基硫代乙内酰脲化合物

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115724759A (zh) * 2022-11-23 2023-03-03 爱斯特(成都)生物制药股份有限公司 一种恩扎卢胺中间体的制备方法
CN116444444A (zh) * 2023-03-27 2023-07-18 盐城工业职业技术学院 一种制备2-取代喹唑啉酮类化合物的方法

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* Cited by examiner, † Cited by third party
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EP3666772A4 (en) 2017-08-07 2021-01-20 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. DIARYLTHIOHYDANTOIN COMPOUND AS ANDROGEN RECEPTOR ANTAGONIST
CN109422737B (zh) * 2017-08-22 2021-07-30 上海时莱生物技术有限公司 咪唑酮类雄激素受体拮抗剂、其制备方法和用途
BR112021015122A2 (pt) * 2019-02-01 2021-09-28 Chia Tai Tianqing Pharmaceutical Group Co., Ltd Cristal de composto de diariltio-hidantoína
CN110452166A (zh) * 2019-09-06 2019-11-15 浙江朗华制药有限公司 一种5-异硫氰酰基-3-三氟甲基-2-氰基吡啶的制备方法
CN114929702B (zh) * 2020-01-19 2024-05-31 正大天晴药业集团股份有限公司 作为ar拮抗剂的二芳基硫代乙内酰脲化合物
CN120112517A (zh) * 2022-10-28 2025-06-06 南京明德新药研发有限公司 桥环类化合物及其在药学上的应用

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WO2015018356A1 (zh) 2013-08-08 2015-02-12 上海医药集团股份有限公司 二芳基乙内酰脲衍生物、其制备方法、药物组合物和应用
CN104341352A (zh) * 2013-08-09 2015-02-11 南京衡杰生物科技有限公司 作为雄激素受体拮抗剂的二芳基乙内酰脲化合物及其应用
CN104341342B (zh) 2014-10-23 2016-04-13 中国电子科技集团公司第四十六研究所 一种高产率、高纯度的dast源粉合成工艺
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TWI726969B (zh) * 2016-01-11 2021-05-11 比利時商健生藥品公司 用作雄性激素受體拮抗劑之經取代之硫尿囊素衍生物
CN110023297A (zh) 2016-07-08 2019-07-16 詹森药业有限公司 作为雄性激素受体拮抗剂的取代的乙内酰脲和硫代己内酰脲衍生物
RU2019108092A (ru) * 2016-08-22 2020-09-22 Янссен Фармацевтика Нв Тиогидантоиновые антагонисты андрогеновых рецепторов для лечения рака
EP3666772A4 (en) 2017-08-07 2021-01-20 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. DIARYLTHIOHYDANTOIN COMPOUND AS ANDROGEN RECEPTOR ANTAGONIST
CN109422737B (zh) * 2017-08-22 2021-07-30 上海时莱生物技术有限公司 咪唑酮类雄激素受体拮抗剂、其制备方法和用途
BR112021015122A2 (pt) 2019-02-01 2021-09-28 Chia Tai Tianqing Pharmaceutical Group Co., Ltd Cristal de composto de diariltio-hidantoína
CN114929702B (zh) * 2020-01-19 2024-05-31 正大天晴药业集团股份有限公司 作为ar拮抗剂的二芳基硫代乙内酰脲化合物

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115724759A (zh) * 2022-11-23 2023-03-03 爱斯特(成都)生物制药股份有限公司 一种恩扎卢胺中间体的制备方法
CN116444444A (zh) * 2023-03-27 2023-07-18 盐城工业职业技术学院 一种制备2-取代喹唑啉酮类化合物的方法

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EP3666772A1 (en) 2020-06-17
JP7285838B2 (ja) 2023-06-02
CN113582977A (zh) 2021-11-02
US11332465B2 (en) 2022-05-17
US20200277290A1 (en) 2020-09-03
CN111032644B (zh) 2021-08-10
KR102658095B1 (ko) 2024-04-19
KR20200043407A (ko) 2020-04-27
EP3666772A4 (en) 2021-01-20
JP2020530490A (ja) 2020-10-22
WO2019029521A1 (zh) 2019-02-14
CA3072269A1 (en) 2019-02-14
AU2018314980A1 (en) 2020-03-05
US11866433B2 (en) 2024-01-09
CN113582977B (zh) 2023-04-14
CN111032644A (zh) 2020-04-17
AU2018314980B2 (en) 2022-05-19
US20230035184A1 (en) 2023-02-02

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